Dextran successful carrier molecule for the delivery of NSAIDs with reduced gastrointestinal effect

Abstract

The dextran ester polymeric prodrug of aceclofenac and mefenamic acid was synthesized through carbonyldiimidazole coupling agent. The prepared polymeric prodrug was characterized by UV, IR, X-RD and 1H NMR. The in vitro hydrolysis study was performed by HPLC and polymeric conjugate subjected for in vitro hydrolysis showed negligible hydrolysis in simulated gastric fluid pH 1.2 for 3 h. The half-life of the aceclofenac dextran conjugate in simulated intestinal fluid (SIF) pH 7.4 and phosphate buffer solution (PBS) pH 9.0 was found to be 8.51 h and 33.72 min, respectively. The half-life 4.66 h and 25.4 min was found in SIF pH 7.4 and PBS pH 9.0, respectively for mefenamic acid conjugates. The conjugates were screened for biological activity such as anti-inflammatory, analgesic and ulcerogenic activity. The statistical data obtained from the biological experiment suggested that the value was found to be significant with respect to normal control.